Document Report Card

ID: ALA1144873

Journal: J Med Chem

Title: An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.

Authors: Watson KG, Brown RN, Cameron R, Chalmers DK, Hamilton S, Jin B, Krippner GY, Luttick A, McConnell DB, Reece PA, Ryan J, Stanislawski PC, Tucker SP, Wu WY, Barnard DL, Sidwell RW.

Abstract: A series of capsid-binding compounds was screened against human rhinovirus (HRV) using a CPE based assay. The ethyl oxime ether 14 was found to have outstanding anti-HRV activity (median IC(50) 4.75 ng/mL), and unlike the equivalent ethyl ester compound 3 (Pirodavir), it has good oral bioavailability, making it a promising development candidate. Compound 14 illustrates that an oxime ether group can act as a metabolically stable bioisostere for an ester functionality.

CiteXplore: 12852746

DOI: 10.1021/jm0202876